Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1999-01-27
2001-04-10
Jones, Dwayne C. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
Reexamination Certificate
active
06214843
ABSTRACT:
TECHNICAL FIELD
The present invention relates to a pharmaceutical composition for the prophylaxis and/or therapy of ischemic intestinal lesions and/or ileus which comprises an adenosine antagonist compound or a salt thereof as an active ingredient and is useful in the pharmaceutical field.
BACKGROUND ART
Not heretofore known is an effective drug for the prevention and treatment of ischemic intestinal lesions and ileus.
DISCLOSURE OF INVENTION
While, in the field of medical care, there is a constant demand for an effective prophylactic or therapeutic drug for ischemic intestinal lesions and ileus, the present invention has for its object to meet this demand.
The inventors of the present invention discovered for the first time that a pyrazolopyridine compound, which is an adenosine antagonist, is effective in the prevention and/or treatment of ischemic intestinal lesions and ileus and have accordingly developed the present invention. The present invention, therefore, provides a pharmaceutical composition comprising said adenosine antagonist compound or salt as an active ingredient to thereby meet the above-mentioned demand.
The pharmaceutical composition of the present invention is implemented by producing a composition comprising a certain adenosine-antagonizing pyrazolopyridine compound or a salt thereof as an active ingredient, which composition is adapted for the prevention or/and treatment of ischemic intestinal lesions and/or ileus, and administering it to a man or animal.
The pyrazolopyridine compound to be used in accordance with the present invention includes pyrazolopyridine compounds of the following general formula (I) or their salts.
[wherein R
1
is lower alkyl, aryl which may have one or more suitable substituent(s), or heterocyclic group;
R
2
is a group of the formula:
(wherein R
4
is protected amino or hydroxy and R
5
is hydrogen or lower alkyl):
cyano;
a group of the formula: —A—R
6
(wherein R
6
is acyl and A is a lower aliphatic hydrocarbon group which may have one or more suitable substituent(s));
amidated carboxy;
unsaturated heterocyclic group which may have one or more suitable substituents;
amino; or
protected amino; and
R
3
is hydrogen, lower alkyl, lower alkoxy, or halogen]
As examples of said pyrazolopyridine compound (I) there can be mentioned those known compounds which are disclosed in Japanese Kokai Tokkyo Koho S64-45385, Kokai Tokkyo Koho H2-243689, Kokai Tokkyo Koho H4-253978, Kokai Tokkyo Koho H5-112566, and WO 95/18128.
The salt of pyrazolopyridine compound (I) preferred for purposes of the present invention is a pharmaceutically acceptable conventional salt and as such includes but is not limited to metal salts such as salts with alkali metals, e.g. sodium salt, potassium salt, etc., and salts with alkaline earth metals, e.g. calcium salt, magnesium salt, etc., ammonium salt, salts with organic bases, e.g. trimethylamine salt, triethylamine salt, pyridine salt, picoline salt, dicyclohexylamine salt, N,N′-dibenzylethylenediamine salt, etc., salts with organic acids, e.g. acetate, trifluoroacetate, maleate, tartrate, fumarate, methanesulfonate, benzenesulfonate, formate, toluenesulfonate, etc., salts with inorganic acids, e.g. hydrochloride, hydrobromide, hydroiodide, sulfate, phosphate, etc., and salts with amino acids such as arginine, aspartic acid, glutamic acid, etc.
REFERENCES:
patent: 64-45385 (1989-02-01), None
patent: 2-243689 (1990-09-01), None
patent: 3-141222 (1991-06-01), None
patent: 4-253978 (1992-09-01), None
patent: 4-244084 (1992-09-01), None
patent: 5-112566 (1993-05-01), None
patent: 6-192092 (1994-07-01), None
patent: 7-33769 (1995-02-01), None
patent: WO 95/18128 (1995-07-01), None
patent: 8-12673 (1996-01-01), None
patent: 8-500338 (1996-01-01), None
patent: 8-99976 (1996-04-01), None
patent: WO 95/18128 (1995-07-01), None
Abstract to JP 3-141222 possessing a publication date of Jun. 17, 1991.
Kadowaki Makoto
Tomoi Masaaki
Fujitsawa Pharmaceutical Co., Ltd.
Jones Dwayne C.
Oblon & Spivak, McClelland, Maier & Neustadt P.C.
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